کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1372967 | 981886 | 2011 | 4 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Synthesis of new opioid derivatives with a propellane skeleton and their pharmacology: Part 1
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موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
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چکیده انگلیسی
The observation that 17-cyclopropylmethylmorphinan derivatives without the 4,5-epoxy ring showed more κ selectivity than those with a 4,5-epoxy ring led us to develop a working hypothesis: the position of the plane composed of the A and B rings would influence the opioid receptor type selectivity and that the decrease in the torsion angle C11–C12–C13–C14 could improve the κ selectivity. Consistent with our hypothesis, KNT-42 with an N-cyclopropylmethyl propellane structure, whose A and B rings were fixed in a torsion angle of approximately 0°, showed κ selective agonist activity.
Propellane derivative KNT-42 showed rather κ selective agonist activity.Figure optionsDownload as PowerPoint slide
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 21, Issue 13, 1 July 2011, Pages 4104–4107
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 21, Issue 13, 1 July 2011, Pages 4104–4107
نویسندگان
Naoshi Yamamoto, Hideaki Fujii, Toru Nemoto, Ryo Nakajima, Shinobu Momen, Naoki Izumimoto, Ko Hasebe, Hidenori Mochizuki, Hiroshi Nagase,